scholarly journals Multiple C–H Activation Enabled Modular Construction of Densely Functionalized Sulfur-Contained Arenes

2021 ◽  
Author(s):  
Wensen Ouyang ◽  
Jianhang Rao ◽  
Jie Wang ◽  
Yang Gao ◽  
Yanping Huo ◽  
...  
Keyword(s):  
Biologically Active ◽  
New Drugs ◽  
Advanced Materials ◽  
Synthetic Chemistry ◽  
Modular Construction ◽  
Judicious Choice ◽  
Directing Group ◽  
Synthetic Application ◽  
Molecular Libraries

<div> <p>Modular construction of multiple functionalized arenes from abundant feedstocks, stands as an unremitting pursue goal in synthetic chemistry, which would accelerate the discovery of new drugs an advanced materials. Herein, by using multiple C-H activation strategy, through judicious choice of versatile imidate ester as the key directing group, expedi-ent delivery of molecular libraries of densely functionalized sulfur-contained arenes. Further synthetic application was demonstrated by multiple C-H modification of fused arenes and pharmaceuticals such as Ibuprofen, and concise con-struction of biologically active molecules, Madam dihydrochloride and Bipenamol, was also achieved.</p> </div> <br>

scholarly journals Multiple C–H Activation Enabled Modular Construction of Densely Functionalized Sulfur-Contained Arenes

2021 ◽  
Author(s):  
Wensen Ouyang ◽  
Jianhang Rao ◽  
Jie Wang ◽  
Yang Gao ◽  
Yanping Huo ◽  
...  
Keyword(s):  
Biologically Active ◽  
New Drugs ◽  
Advanced Materials ◽  
Synthetic Chemistry ◽  
Modular Construction ◽  
Judicious Choice ◽  
Directing Group ◽  
Synthetic Application ◽  
Molecular Libraries

<div> <p>Modular construction of multiple functionalized arenes from abundant feedstocks, stands as an unremitting pursue goal in synthetic chemistry, which would accelerate the discovery of new drugs an advanced materials. Herein, by using multiple C-H activation strategy, through judicious choice of versatile imidate ester as the key directing group, expedi-ent delivery of molecular libraries of densely functionalized sulfur-contained arenes. Further synthetic application was demonstrated by multiple C-H modification of fused arenes and pharmaceuticals such as Ibuprofen, and concise con-struction of biologically active molecules, Madam dihydrochloride and Bipenamol, was also achieved.</p> </div> <br>

scholarly journals Australian microbial biodiscovery: from bugs to drugs

2010 ◽  
Vol 31 (2) ◽  
pp. 74
Author(s):  
Robert J Capon
Keyword(s):  
Drug Discovery ◽  
Biologically Active ◽  
New Drugs ◽  
Medical Need ◽  
Modern Drug ◽  
Drug Discovery Program ◽  
Microbial Natural Products ◽  
Molecular Libraries ◽  
Discovery Pipeline

To maintain and improve the quality of life offered by modern healthcare requires an ongoing commitment to the development of new drugs, to improve and replace those that have become less effective, and to bring to the community safer treatments for an ever-wider array of important diseases. Irrespective of the specific medical need, the drug discovery pipeline is critically dependent on access to diverse, high-quality molecular libraries capable of inspiring drug-led discovery, and ultimately new drugs. A poor choice of chemistry leads to wasted resources and no drugs. Historically the pharmaceutical industry has relied heavily on microbial natural products, which represent an extraordinarily diverse, preassembled pool of biologically active molecules, programmed to be potent and selective modulators of key biopolymers, cells, tissues, organs and animals. Knowledge of Nature?s intellectual property, gleaned from the evolutionary equivalent of a billion-year global drug discovery program, with an unlimited budget and a workforce of trillions, can disclose privileged bioactive structures that inform, guide and inspire modern drug discovery, re-purposing ecological advantage to pharmaceutical benefit.

Oxazole-Based Compounds As Anticancer Agents

2020 ◽  
Vol 26 (41) ◽  
pp. 7337-7371 ◽  
Author(s):  
Maria A. Chiacchio ◽  
Giuseppe Lanza ◽  
Ugo Chiacchio ◽  
Salvatore V. Giofrè ◽  
Roberto Romeo ◽  
...  
Keyword(s):  
Cancer Research ◽  
Drug Discovery ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Chemical Diversity ◽  
Biologically Active ◽  
New Drugs ◽  
The Core ◽  
Anti Cancer ◽  
Biologically Active Derivatives

: Heterocyclic compounds represent a significant target for anti-cancer research and drug discovery, due to their structural and chemical diversity. Oxazoles, with oxygen and nitrogen atoms present in the core structure, enable various types of interactions with different enzymes and receptors, favoring the discovery of new drugs. Aim of this review is to describe the most recent reports on the use of oxazole-based compounds in anticancer research, with reference to the newly discovered iso/oxazole-based drugs, to their synthesis and to the evaluation of the most biologically active derivatives. The corresponding dehydrogenated derivatives, i.e. iso/oxazolines and iso/oxazolidines, are also reported.

scholarly journals What Can Electrochemical Methods Offer in Determining DNA–Drug Interactions?

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3478
Author(s):  
Sandra Ramotowska ◽  
Aleksandra Ciesielska ◽  
Mariusz Makowski
Keyword(s):  
Dna Sequences ◽  
Electrode Materials ◽  
High Reliability ◽  
Electrochemical Methods ◽  
Biologically Active ◽  
New Drugs ◽  
Binding Modes ◽  
Voltammetric Techniques ◽  
Experimental Approaches ◽  
Cellular Dna

The interactions of compounds with DNA have been studied since the recognition of the role of nucleic acid in organisms. The design of molecules which specifically interact with DNA sequences allows for the control of the gene expression. Determining the type and strength of such interaction is an indispensable element of pharmaceutical studies. Cognition of the therapeutic action mechanisms is particularly important for designing new drugs. Owing to their sensitivity, simplicity, and low costs, electrochemical methods are increasingly used for this type of research. Compared to other techniques, they require a small number of samples and are characterized by a high reliability. These methods can provide information about the type of interaction and the binding strength, as well as the damage caused by biologically active molecules targeting the cellular DNA. This review paper summarizes the various electrochemical approaches used for the study of the interactions between pharmaceuticals and DNA. The main focus is on the papers from the last decade, with particular attention on the voltammetric techniques. The most preferred experimental approaches, the electrode materials and the new methods of modification are presented. The data on the detection ranges, the binding modes and the binding constant values of pharmaceuticals are summarized. Both the importance of the presented research and the importance of future prospects are discussed.

scholarly journals Betanin: a promising molecule for biomedical applications

2020 ◽  
Vol 10 (3) ◽  
pp. 5392-5399
Keyword(s):  
Positive Impact ◽  
Pharmaceutical Products ◽  
Free Radical Scavenger ◽  
Biologically Active ◽  
New Drugs ◽  
Radical Scavenger ◽  
Therapeutic Effects ◽  
Pharmacological Properties ◽  
Natural Colorant ◽  
Anti Oxidant

Plants with medicinal properties possess beneficial influences on health and disease. Different plant parts and extracts carry valuable active ingredients with pharmacological properties that lead to developing new drugs. Terminalia bellirica is among those plants that have been formulated as pharmaceutical products. This is attributed to its biologically active phenolics and tannins exhibiting analgesic, anti-hypertensive, anti-microbial, anti-diabetic, anti-oxidant, as well as, other pharmacological properties. Beetroot has been shown to be rich in nitrates with a positive impact on the cardiovascular system. Beetroot contains a number of useful ingredients as the free-radical scavenger ascorbic acid, the anti-inflammatory flavonoids and the anti-oxidant carotenoids. Moreover, beetroot is rich in the natural colorant betalains that are further classified into betacyanins and betaxanthins. Betanin, is one of the major constituents of beetroots that have been postulated to possess significant beneficial therapeutic effects in a number of conditions and diseases. However, several studies have demonstrated the relatively poor bioavailability of betanin upon oral administration. In the current review we aim to highlight some of the latest researches dealing with the therapeutic properties of betanin in different disease conditions, the possible mechanistic pathways beyond such beneficial effects and plausible strategies capable of enhancing its stability and bioavailability.

scholarly journals Zinc Chloride Catalyzed Amino Claisen Rearrangement of 1-N-Allylindolines: An Expedient Protocol for the Synthesis of Functionalized 7-Allylindolines

2019 ◽  
Vol 25 (1) ◽  
pp. 22-26 ◽  
Author(s):  
Seema Jain
Keyword(s):  
Zinc Chloride ◽  
Claisen Rearrangement ◽  
Reaction System ◽  
Biologically Active ◽  
Catalyst Loading ◽  
One Pot ◽  
Substitution Pattern ◽  
Claisen Rearrangements ◽  
Lower Temperature ◽  
Molecular Libraries

Abstract7-Allylindolines are valuable synthons for designing biologically active molecular libraries. Lewis acid catalyzed amino-Claisen rearrangement provides a one pot synthetic entry to these heteroarenes. In this context, Zinc chloride (ZnCl2)–N,N-dimethylformamide system efficiently catalyzed amino-Claisen rearrangements of 1-N-allylindolines to 7-allylindolines. The rearrangement is influenced by stereoelectronic effects of substituents present in 1-N-allylindolines. The substrates containing electron donating functionalities underwent rearrangement at lower temperature than substrates with electron withdrawing functional groups. The regioselectivity of the process is governed by the substitution pattern on allyl moiety in 1-N-allylindoline as well as ZnCl2 catalyst loading in the reaction system.

scholarly journals Asymmetric Suzuki-Miyaura coupling of heterocycles via Rhodium-catalysed allylic arylation of racemates

2017 ◽  
Vol 8 (1) ◽  
Author(s):  
Philipp Schäfer ◽  
Thomas Palacin ◽  
Mireia Sidera ◽  
Stephen P. Fletcher
Keyword(s):  
Asymmetric Catalysis ◽  
Anticancer Agent ◽  
Cross Coupling ◽  
Boronic Acids ◽  
Biologically Active ◽  
Advanced Materials ◽  
Industrial Sectors ◽  
Single Isomer ◽  
Carbon Carbon Bonds ◽  
Drug Synthesis

Abstract Using asymmetric catalysis to simultaneously form carbon–carbon bonds and generate single isomer products is strategically important. Suzuki-Miyaura cross-coupling is widely used in the academic and industrial sectors to synthesize drugs, agrochemicals and biologically active and advanced materials. However, widely applicable enantioselective Suzuki-Miyaura variations to provide 3D molecules remain elusive. Here we report a rhodium-catalysed asymmetric Suzuki-Miyaura reaction with important partners including aryls, vinyls, heteroaromatics and heterocycles. The method can be used to couple two heterocyclic species so the highly enantioenriched products have a wide array of cores. We show that pyridine boronic acids are unsuitable, but they can be halogen-modified at the 2-position to undergo reaction, and this halogen can then be removed or used to facilitate further reactions. The method is used to synthesize isoanabasine, preclamol, and niraparib—an anticancer agent in several clinical trials. We anticipate this method will be a useful tool in drug synthesis and discovery.

scholarly journals BIOMIMETIC APPROACHES TO STUDY OF PROPERTIES OF MEDICINAL SUBSTANCES

2019 ◽  
Vol 62 (10) ◽  
pp. 4-29
Author(s):  
Nina B. Melnikova ◽  
Olga N. Solovyova ◽  
Evgeni N. Evgeni N. Kochetkov
Keyword(s):  
Antioxidant Activity ◽  
Superoxide Dismutase ◽  
Lipid Bilayers ◽  
Superoxide Anion ◽  
Molecular Form ◽  
Biologically Active ◽  
New Drugs ◽  
In Vitro Experiments ◽  
Medicinal Substances

The review is devoted to an assessment of the current level of use of biomimetic approaches to the study of the properties of known drugs and the development of new drugs. In this review, we consider the main biological functions of superoxide dismutase, namely the catalytic decomposition of toxic superoxide anion of oxygen to the molecular form of oxygen and protection against induced apoptosis. The biomimetic enzymes-Mn- and TEMPO-containing equivalents of superoxide dismutase SOD with antitumor and antioxidant activity were discussed more detail. The relationship between the properties and activity of SOD mimetics with their structure among them the nature of the anion and ligands, the coordination number, the geometry of the presence of conjugated bonds, and other parameters of the molecules. The study of the properties of Mn-SOD mimetics makes it possible to develop a new class of drugs successfully tested by in vivo and in vitro experiments and which are at the stages of clinical trials. Stable TEMPO radicals containing compounds are able to perform SOD functions, exhibiting antioxidant activity in relation not only to superoxide-anion, but also to peroxynitrile, and moreover to act as a spin label. The biomimetic membrane systems (monolayers, planar lipid bilayers, liposomes and other nano-sized objects) are discussed too for studying properties in in vitro experiments and for delivering potent and medicinal substances. The biomimetic approach combination allows to create the new promising drugs, including those based on SOD mimetics, and to develop the synthetic analogues of biologically active substances and methods of their delivery. The advantages of such dosage forms are lower toxicity of the preparations, lack of immunogenicity and a decrease in the dose of potent drugs.

scholarly journals CHEMICAL CONSTITUENTS OF GEUM RIVALE L. AND THEIR BIOLOGICAL ACTIVITY

2020 ◽  
Vol 8 (2) ◽  
pp. 133-146
Author(s):  
Anastasia A. Orlova ◽  
Maria N. Povydysh
Keyword(s):  
Pharmacological Activity ◽  
Chemical Constituents ◽  
Biologically Active ◽  
New Drugs ◽  
Main Research ◽  
Internet Resources ◽  
Pharmaceutical Substances ◽  
Urgent Task ◽  
Antiviral Activities ◽  
Promising Source

The aim of the study is to review the literature data on the chemical constituents of arial and underground parts of Geum rivale L. (Rosaceae) and the pharmacological activity of its extracts and individual compounds.Materials and methods. The study was carried out using Internet resources (Google Scholar, PubMed) and library databases (e-Library, Scopus, Web of Science). The main research methods were a review and analysis of the literature data on the topic for the period from 1958 up to the present.Results. For the period from 1958 up to the present more than 80 components in the arial and underground parts of G. rivale have been identified.  Among them there were components of the essential oil, phenolic acids and coumarins, aglycones of flavonoids, including luteolin, apigenin, quercetin and kaempferol, as well as a number of their glycosides and glucuronides, ellagitannins (hemin A, B, C, D, pedunculagin, stachiurin/casuarinin, tellimagrandin I). Some aspects of the pharmacological activity of total extracts and individual secondary metabolites of G. rivale have been studied, anti-inflammatory, antioxidant, antimicrobial, antiviral activities have been experimentally confirmed.Conclusion. The analysis of the literature data showed that a further study of the composition of metabolites of G. rivale and their pharmacological activity is an urgent task, the solution of which will expand the range of use of this plant in medical practice and consider G. rivale as a promising source of pharmaceutical substances for the creation of new drugs and biologically active additives.

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